LTE4 [Ligand Id: 3352] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL509456
  • ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
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  • CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
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  • CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
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  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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  • GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.055 uM) in membrane vesicles from Mrp2-expressing Sf9 cells F 5.01 pIC50 9830 nM IC50 Mol Pharmacol (2001) 59: 1077-1085 [PMID:11306690]
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb - - 7.8 pKi - - - Mol Pharmacol (1998) 53: 750-8 [PMID:9547367]
GtoPdb - - 6.97 pIC50 107 nM IC50 Nature (1999) 399: 789-93 [PMID:10391245]
GtoPdb - - 6.41 pEC50 391 nM EC50 Mol Pharmacol (2011) 79: 270-8 [PMID:21078884]
GtoPdb - - 6.67 pEC50 212 nM EC50 Nature (1999) 399: 789-93 [PMID:10391245]
ChEMBL Agonist activity at human CysLT1 receptor F 6.98 pEC50 104 nM EC50 J Med Chem (2021) 64: 16512-16529 [PMID:34767347]
GtoPdb - - 7.24 pEC50 58 nM EC50 Mol Pharmacol (1999) 56: 657-63 [PMID:10462554];
Biochem Biophys Res Commun (2000) 274: 316-22 [PMID:10913337];
Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
GtoPdb - - 6.5 pKi - - - Mol Pharmacol (1998) 53: 750-8 [PMID:9547367]
GtoPdb - - 5.72 pIC50 1890 nM IC50 Biochem Biophys Res Commun (2000) 274: 316-22 [PMID:10913337]
GtoPdb - - 6.16 pIC50 693 nM IC50 J Biol Chem (2000) 275: 30531-6 [PMID:10851239];
Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]
GtoPdb - - 5.92 pEC50 1208 nM EC50 J Biol Chem (2000) 275: 30531-6 [PMID:10851239];
Mol Pharmacol (2011) 79: 270-8 [PMID:21078884]
ChEMBL Agonist activity at human CysLT2 receptor F 6.53 pEC50 293 nM EC50 J Med Chem (2021) 64: 16512-16529 [PMID:34767347]
GtoPdb - - 7.11 pEC50 77 nM EC50 Biochem Biophys Res Commun (2000) 274: 316-22 [PMID:10913337];
Mol Pharmacol (2000) 58: 1601-8 [PMID:11093801]
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
ChEMBL Agonist activity at human P2Y12 receptor F 8.89 pEC50 1.3 nM EC50 J Med Chem (2009) 52: 5803-5815 [PMID:19739647]
GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
GtoPdb - - 9.51 pEC50 0.31 nM EC50 PLoS ONE (2008) 3: e3579 [PMID:18974869]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]